Visible‐Light Mediated Photooxidative Phosphorylation of Benzylamines: A Novel and Mild Pathway Towards α‐Aminophosphorus Compounds

Abstract Traditional syntheses of α‐aminophosphorus therapeutic targets proceed through the hydrophosphorylation of C=N or C=O bonds, thus necessitating preliminary oxidized substrates. Cross‐dehydrogenative coupling strategies can bypass this extra oxidation step by oxidizing simpler substrates in situ before phosphorylating them, but those protocols can suffer from the use of toxic stoichiometric oxidants. Photochemical strategies can access those oxidized intermediates without any harsh conditions and can use molecular oxygen as a benign and sustainable oxidant. We report herein a simple protocol using visible light, phosphinylidenes and benzylamine derivatives for the synthesis of α‐aminophosphorus products under aerobic conditions and using an iridium photosensitizer.